CAS: 244105-55-3; 4-Amino-1-((2R,3R,4R,5R)-4-Hydroxy-5-(Hydroxymethyl)-3-(2-Methoxyethoxy)Tetrahydrofuran-2-yl)-5-Methylpyrimidin-2(1H)-One

该化合物是一个经过修改的核糖核素底,配有特定的烷基和乙醚替代品,该化合物的特点是,在细胞环的5处存在一个可以影响其生物活动和稳定性的甲基组,这可能会影响其生物活动和稳定性.2'thoxythoxy类组会提高溶解性,并可能改善化合物的药理特性,使其在治疗应用中可能有用,特别是在核酸化学和药物开发领域.这些改变会影响核糖核素与酶的相互作用,并会将其纳入核酸中,这对于其在生物系统中的功能至关重要.此外,该化合物在结合性和特性方面可能会表现出独特的特性,因此它成为与基因调节和肾学有关的研究的一个主题.

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113886-70-7 223777-16-0 2140-61-6

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    专利信息


    专利号:US-7002006-B2
    优先权日:2003-02-12
    标 题:Protection of nucleosides
    发明人:SONG QUANLAI; ROSS BRUCE S
    权利人:ISIS PHARMACEUTICALS INC
    摘要:A process of manufacturing protected nucleosides comprises reacting a nucleoside with a protecting reagent in the presence of a regioselective activator to produce a regioselectively protected nucleoside. In some embodiments of the inventive method, an optionally substituted trityl or optionally substituted pixyl group is selectively added to the 5'-O-position of a nucleoside in the presence of lutidine as activator or activator/solvent. The inventive method results in improved selectivity of the 5'-O-position over the 3'-O-position, thereby improving overall product yield and purity, and permitting simplified purification protocols, in some cases obviating the need for chromatography to produce a purified protected nucleoside suitable for automated synthesis of oligonucleotides, such as primers, probes and antisense molecules.

    专利号:US-2015139987-A1
    优先权日:2013-11-20
    标 题 :Treatment of homozygous familial hypercholesterolemia
    发明人:MARTIN ROBERT L; MCWHERTER CHARLES A; O'MARA PATRICK J
    权利人:CYMABAY THERAPEUTICS INC
    摘要:Treatment of homozygous familial hypercholesterolemia by administration of (R)-2-(4-((2-ethoxy-3-(4-(trifluoromethyl)phenoxy)propyl)thio)-2-methylphenoxy)acetic acid or a salt thereof, optionally in combination with an MTP inhibitor, an apoB-100 synthesis inhibitor, or a PCSK9 inhibitor.

    专利号:US-12338436-B2
    优先权日:2018-06-29
    标题 :Synthetic guide molecules, compositions and methods relating thereto
    发明人:SACCOMANO SAM; CAPEHART STACY; EATON BRUCE; BERRY KARIN ZEMSKI
    权利人:EDITAS MEDICINE INC
    摘要:Chemical syntheses of guide molecules are disclosed, along with compositions and methods relating thereto. A cost-effective and straightforward chemical synthesis of high-purity unimolecular guide molecules with minimal n−1 and/or n+1 species, truncation species, and other contaminants by providing, among other things, methods for synthesizing unimolecular guide molecules that involve cross-linking two or more pre-annealed guide fragments.

    专利号:CN-118047824-A
    优先权日:2024-04-01
    标 题:Application of dialkylphosphonic acid in oligonucleotide synthesis

    专利号:CN-118047824-B
    优先权日:2024-04-01
    标题 :Application of dialkylphosphonic acid in oligonucleotide synthesis
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    主要参考文献

    参考标题:Protection Of Nucleosides
    摘要:A Process Of Manufacturing Protected Nucleosides Comprises Reacting A Nucleoside With A Protecting Reagent In The Presence Of A Regioselective Activator To Produce A Regioselectively Protected Nucleoside. In Some Embodiments Of The Inventive Method, An Optionally Substituted Trityl Or Optionally Substituted Pixyl Group Is Selectively Added To The 5′-O-Position Of A Nucleoside In The Presence Of Lutidine As Activator Or Activator/solvent. The Inventive Method Results In Improved Selectivity Of The 5′-O-Position Over The 3′-O-Position, Thereby Improving Overall Product Yield And Purity, And Permitting Simplified Purification Protocols, In Some Cases Obviating The Need For Chromatography To Produce A Purified Protected Nucleoside Suitable For Automated Synthesis Of Oligonucleotides, Such As Primers, Probes And Antisense Molecules.
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